2,4,5-Triphenylisothiazol-3(2H)-one 1,1-dioxides as inhibitors of human leukocyte elastase.

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dc.contributor.authorGutschow, M.
dc.contributor.authorPietsch, M.
dc.contributor.authorThemann, A.
dc.contributor.authorFahrig, J.
dc.contributor.authorSchulze, B.
dc.date.issued2005
dc.description.abstractA series of substituted 2,4,5-triphenylisothiazol-3(2H)-one 1,1-dioxides 9 was synthesized and investigated as inhibitors of human leukocyte elastase (HLE). All compounds were found to inhibit HLE in a time-dependent manner and most of them exhibited kobs/[I] values > 300 M− 1s− 1. The most potent 3-oxosultam of this series was 9l (kobs/[I] = 2440 M− 1s− 1). Kinetic investigations performed with 9g and different substrate concentrations did not allow to clearly distinguish between a competitive or noncompetitive mode of inhibition. A more complex interaction is supported by the failure of a linear dependency of kobs values on the inhibitor concentration.
dc.description.statementofresponsibilityMichael Gütschow, Markus Pietsch, Andrea Themann, Janine Fahrig‌and Bärbel Schulze‌
dc.description.urihttp://informahealthcare.com/doi/abs/10.1080/14756360500148783?journalCode=enz
dc.identifier.citationJournal of Enzyme Inhibition and Medicinal Chemistry, 2005; 20(4):341-347
dc.identifier.doi10.1080/14756360500148783
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.urihttp://hdl.handle.net/2440/55847
dc.language.isoen
dc.publisherInforma Healthcare
dc.source.urihttp://dx.doi.org/10.1080/14756360500148783
dc.title2,4,5-Triphenylisothiazol-3(2H)-one 1,1-dioxides as inhibitors of human leukocyte elastase.
dc.typeJournal article
pubs.publication-statusPublished

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